sedative-hypnotic-anxiolytics: benzodiazepines & others tracy a. womble, ph.d florida a&m...
TRANSCRIPT
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Sedative-Hypnotic-Anxiolytics:Benzodiazepines & others
Tracy A. Womble, Ph.D
Florida A&M University
College of Pharmacy and Pharmaceutical Sciences
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SEDATIVE-HYPNOTICS
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History of Sedatives
• Alcohol, the oldest known sedative– “When Noah left the Ark he planted a
vineyard, drank the wine, and was drunken, and he was uncovered within his tent.” Genesis 9:21
• 1900 Barbiturates: narrow TI • 1960’s Chlordiazepoxide (Librium)
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SEDATIVE-HYPNOTIC DRUGSSEDATIVE-HYPNOTIC DRUGS
SEDATION• Reduction of anxiety• Calming effectANXIOLYTIC• Drug that reduces anxiety• SedativeHYPNOSIS• Induce sleep
– go to sleep fast, feel refreshed tomorrow !!!
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What is Anxiety ?
• an unpleasant state of tension, apprehension, or uneasiness; a fear that seems to arise from a sometimes unknown source.
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Classification of Anxiety Disorders
• Generalized Anxiety Disorder (GAD)• Panic Disorder• Social Phobia• Simple Phobia • Obsessive Compulsive Disorder (OCD)
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Classification of Anxiety Disorders
Generalized Anxiety Disorder (GAD) exaggerated autonomic response, irritability, difficulty in concentrating and swallowing, and insomnia.
Panic Disorder - autonomic symptoms, hot flashes, and fear of dying or going crazy.
Social Phobia - fear of eating, writing or speaking in public.
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Simple Phobia - Phobias of heights, animals, driving, or air travel.
Obsessive Compulsive Disorder (OCD) :• Obsessions are persistent ideas
– e.g., recurrent thoughts of contamination.• Compulsions are repetitive behaviors
– e.g., repetitive hand-washing.
• Significantly interfere with the patient’s social and practical life.
Classification of Anxiety Disorders (Cont)
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Anxiolytics
• Benzodiazepines• Buspirone• SSRIs (Those FDA approved for
Anxiety)• SNRIs (Those approved for Anxiety)• Hydroxyzine• Clomipramine
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Sedative/Hypnotic/Anxiolytic
• Because many of the antianxiety drugs also cause some sedation, the same drugs often function clinically as both anxiolytic and hypnotic (sleep-inducing) agents.
• In addition, some have anticonvulsant activity.
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Dose Response Curve for Sedative/Hypnotics
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EFFECTIVE SEDATIVE-HYPNOTIC DRUGS
EFFECTIVE SEDATIVE-HYPNOTIC DRUGS
• Lipid soluble• Absorbed well from the GIT• Good distribution to the brain• Metabolized before elimination from the
body
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SEDATIVE-HYPNOTIC DRUGSSEDATIVE-HYPNOTIC DRUGS
Benzodiazepines Barbiturates Miscellaneous agents
Short Ultra short
acting acting
Intermediate Short Buspirone
acting acting Chloral hydrate
Long Long Zaleplon
acting acting Zolpidem
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Actions of Sedative Hypnotics• Sedation / Anxiolytics
– Amnesia during surgical procedure
• Hypnosis (insomnia)• Adjunct to Anesthesia • Anticonvulsant effects (i.v.)• Muscle Relaxation• Respiration and Cardiovascular• Control of ethanol, sedative-hypnotic
withdrawal
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Action Potential of a Neuron
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SEDATIVE-HYPNOTIC DRUGSSEDATIVE-HYPNOTIC DRUGS
BENZODIAZEPINES• receptors
Form part of GABAA receptor-chloride ion channel macromolecular structure
Binding facilitates the inhibitory actions of GABA
Increased GABA mediated chloride ion conductance
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Benzodiazepine Receptor• Located on the GABAA receptor
– Divided into 3 main types (A,B and C)• GABA A,B,C
– GABA A - ligand-gated Cl- ion channel (ionotropic)• GABA,B,C are metabotropic
• Hippocampus, striatum, spinal cord, mediate anxiolysis– Most common throughout CNS, mediate
sedation
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Benzodiazepine Indications• Sedation/Hypnotic
• Anxiety
• Anesthesia
• Alcohol withdrawal syndrome
• Anticonvulsant
• Muscular disorders
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Benzodiazepine Receptor
• Ionotropic receptor – (GABAA) form ion channels– Metabotropic receptor – (GABAB ) BZP’s have very
low affinity for GABAB
• GABAA receptor- contains 5 subunits found in many regions of brain, different regions of CNS
• contain different combinations– (6) α, (3) β, (3) γ and (2) δ
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Benzodiazepines (BZP) Mechanism of Action
• BZP receptor linked to GABAA receptor complex (bound to Cl- channels). – BZP enhance GABAA effect.
– GABA: an inhibitory neurotransmitter
• Open Cl- channels in response to GABA activation, hyperpolarization, decrease neuronal firing
• Effects: Sedative, Hypnotic, Anticonvulsant, Muscle-Relaxant, Anxiolytic
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Pharmacokinetics of Benzodiazepines
• Lipid-soluble: fast cross blood-brain-barrier: rapid onset of action. – obese, elderly
• Biotransformation & Half-Life: – Hepatic oxidation: long-t½, active
metabolites– Glucuronidation: short-t½, no active metab.
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Pharmacokinetics of Benzodiazepines Pharmacokinetics of Benzodiazepines
• Diazepam, Chlordiazepoxide, Clorazepate
and Flurazepam – Converted initially to active metabolites with long
half-lives
After several days of therapy accumulation of active metabolites can lead to excessive sedation
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Pharmacokinetics of Benzodiazepines Pharmacokinetics of Benzodiazepines
BENZODIAZEPINES
• Diazepam, Chlordiazepoxide, Clorazepate*desmethyldiazepam active
oxazepam metabolites
conjugation
* Prodrug
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SEDATIVE-HYPNOTIC DRUGSSEDATIVE-HYPNOTIC DRUGS
BENZODIAZEPINES• Lorazepam and oxazepam
Undergo extrahepatic conjugation and do not form active metabolites
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Biotransformation of BZPs
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Benzodiazepine Classification Half Life (t½) (hrs.) Therapeutic Use
Midazolam(Versed)
Short Acting 2-6 Preanesthetic, intraoperative
Triazolam(Halicon)
Short Acting 2-3 Insomnia
Alprazolam(Xanax)
Intermediate Acting 12-15 Anxiolytic, agoraphobia
Estazolam(Prosom)
Intermediate Acting 10-24 Insomnia
Lorazepam(Ativan)
Intermediate Acting 10-20 Anxiolytic, preanesthetic
Temazepam(Restoril)
Intermediate Acting 10-40 Insomnia
Clonazepam(Klonipin)
Long Acting 18-50 Anticonvulsant
Clorazepate(Tranxene)
Long Acting 40-50 Anxiolytic, anticonvulsant
Diazepam(Valium)
Long Acting 20-80 Anxiolytic, status epilepticus, muscle relaxant, anesthetic
premed
Flurazepam(Dalmane)
Long Acting 40-100 Insomnia
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BZD: Adverse Effects• BZD few SE • Sedation, CNS Depression
– Worse if combined with EtOH• Behavioral disinhibition
– Irritab, excitement, aggression • Psychomotor & Cognitive Impairment
– coordination, attention (driving)– poor visual-spatial ability (not aware of it)– Ataxia, confusion
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BZD: Adverse Effects• Overdose: Rare fatalities if BZD
alone
• Hypnotic dose of BZP may worsen snoring/OSA
• Severe CNS & Respiratory Depression if combined –alcohol, barbiturates, narcotics,TCA’s
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Benzodiazepine AntagonistBenzodiazepine Antagonist• Flumazenil (Romazicon)
Reverses the CNS effects of benzodiazepines, Eszopiclone, Zaleplon and Zolpidem
Antagonist at the BZP receptor, no effect on barbiturates.
Management of BZP overdose
t½ 0.7-1.3 hr – sedation commonly recurs, requires repeated admin.
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Barbiturates• Not used for anxiety or insomnia
– Used for induction of anesthesia
• Potentially Fatal Respiratory Depression– narrow TI
• Induce P450 system: interactions
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Barbiturates• Gen Anesthesia (induction) - thiopental• Sedative - Amobarbital, pentobarbital• Anticonvulsant – Phenobarbital
• Abrupt withdrawal after physical dependence may result in death
• Increase porphyrin synthesis, contraindicated in pts. w/ acute intermittent porphyria
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Action of Barbiturates• CNS–
– Low dose, sedation. High dose, hypnosis, anesthesia, finally coma and death. CNS depression dependent on dose. No analgesic properties.
• Respiratory Depression– Suppress hypoxic and chemoreceptor response to CO2
• Enzyme Induction – induce P450 microsomal enzymes.
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Barbiturate Poisoning• Lethal dose >10x hypnotic dose • Tx of acute barbiturate poisoning is
supportive– Hemodialysis or hemoperfusion– Purging of stomach– Diuresis/alkalinization of urine– Airway ventilation– Gastric lavage if < 24hr since ingestion
• Admin. Activated charcoal to shorten t½
• CNS stimulants contraindicated, increases mortality
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Non-Benzodiazepine Sedative Hypnotics
• Zolpidem (Ambien)• Zaleplon (Sonata)• Eszopiclone (Lunesta• Buspirone (Buspar)• Chloral Hydrate
(Aquachloral)• Propofol (Diprivan)
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Benzodiazepine-Receptor Agonists
• Zolpidem (Ambien), Zaleplon (Sonata), Eszopiclone (Lunesta)
• Structurally similar to BZPs
• Sedation and hypnosis
• Effects reversed by Flumazenil
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Zolpidem (Ambien)• Ambien, Ambien CR, Zolpimist• Acts at subset of BZP receptors• no anticonvulsant or muscle relaxation
properties• no withdrawal effect, Minimal rebound
insomnia, t½ 2-3 hrs,• Little to no tolerance with prolonged use• Adverse effects - nightmares, agitation, h/a,
GI upset, dizziness and daytime drowsiness
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Zaleplon (Sonata)• Similar to Zolpidem hypnotic action
• Less residual s/e on psychomotor and cognitive than zolpidem and BZPs
• Causes fewer cognitive side effects
• t½ < 1 hr.
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Eszopiclone (Lunesta)• Used in tx of insomnia• Effective up to 6 months • Rapidly absorbed (1 hour)• metabolized by oxidation /demethylation• t½ ~ 6 hrs• Adverse effects – anxiety, dry mouth, chest
pain, h/a, migraine, peripheral edema, somnolence, unpleasant taste
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Buspirone (Buspar)• mediated by serotonin ((5-HT1A)
• minimal sedation, no physical dependence or tolerance, no withdrawal
• Not a BZP, not hypnotic, no CNS depression w/ alcohol
• no anticonvulsant or muscle relaxant, minimal sedation
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Buspirone (Buspar)• tx of GAD, onset of action – 1 wk
• Effects not reversed by Flumazenil
• hypothermia, inc. prolactin, GH release
• < motor function interference (important in elderly)
• < nicotine cravings in tobacco users
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Chloral Hydrate• Prodrug - active. metab. inc.
anticoagulant effect– (displace form protein binding site)
• Sedative / hypnotic–onset ~ 30 min. DOA 6 - 10 hrs.
• Irritating to GI tract– Produces unusual, unpleasant taste
sensation, synergizes w/ alcohol
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Propofol (Diprivan)
• i.v. sedative/hypnotic
• induction/maintenance of anesthesis
• smooth onset ~ 40s, facilitates CNS depression
• no postaneshetic n/v